EP4458418A3 - Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer - Google Patents

Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer Download PDF

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Publication number
EP4458418A3
EP4458418A3 EP24194380.2A EP24194380A EP4458418A3 EP 4458418 A3 EP4458418 A3 EP 4458418A3 EP 24194380 A EP24194380 A EP 24194380A EP 4458418 A3 EP4458418 A3 EP 4458418A3
Authority
EP
European Patent Office
Prior art keywords
alpha
cancer
emitting radionuclides
macrocyclic complexes
targeted radiotherapy
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP24194380.2A
Other languages
German (de)
French (fr)
Other versions
EP4458418A2 (en
Inventor
Justin WILSON
Nikki THIELE
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cornell University
Original Assignee
Cornell University
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cornell University filed Critical Cornell University
Publication of EP4458418A2 publication Critical patent/EP4458418A2/en
Publication of EP4458418A3 publication Critical patent/EP4458418A3/en
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/0474Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0482Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1045Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody against animal or human tumor cells or tumor cell determinants
    • A61K51/1051Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody against animal or human tumor cells or tumor cell determinants the tumor cell being from breast, e.g. the antibody being herceptin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00Preparations for use in therapy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1093Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
    • A61K51/1096Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies radioimmunotoxins, i.e. conjugates being structurally as defined in A61K51/1093, and including a radioactive nucleus for use in radiotherapeutic applications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Organic Chemistry (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The present technology generally relates to macrocyclic complexes of alpha-emitting radionuclides, as well as compositions including such compounds and methods of use.
EP24194380.2A 2017-03-30 2018-03-30 Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer Pending EP4458418A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762478945P 2017-03-30 2017-03-30
EP18775715.8A EP3600452B1 (en) 2017-03-30 2018-03-30 Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer
PCT/US2018/025488 WO2018183906A1 (en) 2017-03-30 2018-03-30 Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
EP18775715.8A Division EP3600452B1 (en) 2017-03-30 2018-03-30 Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer

Publications (2)

Publication Number Publication Date
EP4458418A2 EP4458418A2 (en) 2024-11-06
EP4458418A3 true EP4458418A3 (en) 2024-11-13

Family

ID=63676871

Family Applications (2)

Application Number Title Priority Date Filing Date
EP24194380.2A Pending EP4458418A3 (en) 2017-03-30 2018-03-30 Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer
EP18775715.8A Active EP3600452B1 (en) 2017-03-30 2018-03-30 Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer

Family Applications After (1)

Application Number Title Priority Date Filing Date
EP18775715.8A Active EP3600452B1 (en) 2017-03-30 2018-03-30 Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer

Country Status (9)

Country Link
US (2) US11554182B2 (en)
EP (2) EP4458418A3 (en)
JP (2) JP7675500B2 (en)
KR (3) KR20260008174A (en)
CN (1) CN110573186A (en)
AU (1) AU2018243682B2 (en)
ES (1) ES2992988T3 (en)
IL (2) IL311111A (en)
WO (1) WO2018183906A1 (en)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3883610A4 (en) * 2018-11-20 2022-11-02 Cornell University MACROCYCLIC COMPLEXES OF RADIONUKLIDES AND THEIR USE IN CANCER RADIOTHERAPY
WO2020180756A1 (en) * 2019-03-01 2020-09-10 Washington University Compositions and methods for radiotherapy using chelated radiotherapeutic agents and non-target tissue blockade
EA202193076A1 (en) * 2019-05-10 2022-02-16 Янссен Байотек, Инк. MACROCYCLIC CHELATORS AND METHODS FOR THEIR APPLICATION
WO2022101771A1 (en) 2020-11-10 2022-05-19 Janssen Biotech, Inc. Macrocyclic compounds and methods of use thereof
KR20230142482A (en) 2021-01-27 2023-10-11 얀센 바이오테크 인코포레이티드 Immunoconjugates comprising kallikrein-related peptidase 2 antigen-binding domain and uses thereof
GEAP202316335A (en) * 2021-02-01 2023-10-10 Bayer Ag Multimeric chelator compounds for use in targeted radiotherapy
JP2024060110A (en) * 2021-02-19 2024-05-02 住友化学株式会社 Radioactive metal complex and method for producing same
JP2024045789A (en) * 2021-02-19 2024-04-03 住友化学株式会社 Compounds and metal complexes
WO2022249089A1 (en) 2021-05-27 2022-12-01 Janssen Biotech, Inc. Compositions and methods for the treatment of prostate cancer
WO2023026236A1 (en) * 2021-08-27 2023-03-02 Janssen Biotech, Inc. Anti-psma radioconjugates and uses thereof
EP4392454A4 (en) 2021-08-27 2025-10-15 Janssen Biotech Inc ANTI-PSMA ANTIBODIES AND USES THEREOF
CA3240194A1 (en) 2021-11-09 2023-05-19 Edward Cleator Macrocyclic compounds and methods of making the same
WO2023084397A1 (en) 2021-11-09 2023-05-19 Janssen Biotech, Inc. Macrocyclic compounds and diagnostic uses thereof
US20250099635A1 (en) 2022-01-26 2025-03-27 Janssen Biotech, Inc. Iimmunoconjugates comprising kallikrein related peptidase 2 antigen binding domains and their uses
JP2023135733A (en) * 2022-03-16 2023-09-29 Jfeエンジニアリング株式会社 Zirconium complex and its synthesis method
WO2023215293A1 (en) 2022-05-02 2023-11-09 Athanor Biosciences, Inc. Cancer eradicating – bio-nanoparticles (ce-bnp)
WO2023215560A1 (en) 2022-05-05 2023-11-09 Atoosa Corporation Tumor cell/immune cell multivalent receptor engager – bio-nanoparticle (timre-bnp)
EP4279092A1 (en) 2022-05-17 2023-11-22 Bayer AG Radiopharmaceutical complexes targeting prostate-specific membrane antigen
CN119173283A (en) 2022-05-17 2024-12-20 拜耳股份有限公司 Radiopharmaceutical complexes targeting prostate specific membrane antigen and combinations thereof
EP4694938A2 (en) * 2023-04-10 2026-02-18 Board Of Trustees Of Michigan State University Cancer-targeted alpha-particle therapeutic vehicles for treatment of cancer
TW202517674A (en) 2023-10-19 2025-05-01 德商拜耳廠股份有限公司 Anti-gpc3 antibodies and radioconjugates thereof
EP4552657A1 (en) 2023-11-07 2025-05-14 Bayer Aktiengesellschaft Radiopharmaceutical complexes and combinations
DE102024109122A1 (en) 2024-03-28 2025-10-02 Helmholtz-Zentrum Dresden - Rossendorf E. V. 1,4,10,13-Tetraoxa-7,16-diazacyclooctadecane derivatives and their use

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018187631A1 (en) * 2017-04-05 2018-10-11 Cornell University Trifunctional constructs with tunable pharmacokinetics useful in imaging and anti-tumor therapies

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4597903A (en) 1984-08-21 1986-07-01 University Of Maryland Process for the direct preparation of N,N-disubstituted derivatives for 4,13-diaza-18-crown-6
US5747345A (en) 1996-08-15 1998-05-05 Johnson & Johnson Clinical Diagnostics, Inc. Calcium specific diaza-18-crown-6-ether chromoionophores
JP2002098981A (en) * 2000-09-21 2002-04-05 Seiko Epson Corp Liquid crystal device, method of manufacturing the same, and electronic equipment
GB0624587D0 (en) 2006-12-08 2007-01-17 Univ Muenchen Tech Chelating agent
ES2354666B1 (en) * 2009-07-27 2012-01-03 Universidade Da Coruña Y En Su Nombre Y Representacion El Rector Jose Maria Barja Perez COMPOSITE FOR SELECTIVE EXTRACTION OF STRONTIUM (II) AND LEAD (II).
CN103421133A (en) * 2013-08-03 2013-12-04 大连理工大学 Rare-earth metal catalysis system for catalyzing high-stereoregularity polymerization of alpha-olefin
WO2015176056A1 (en) 2014-05-16 2015-11-19 Memorial Sloan Kettering Cancer Center One-step labeling of antibodies to high specific activity with actinium-225
MA41176A (en) 2014-12-17 2017-10-24 Bayer As RADIO-PHARMACEUTICAL COMPLEXES
US10806806B2 (en) * 2016-06-23 2020-10-20 Cornell University Trifunctional constructs with tunable pharmacokinetics useful in imaging and anti-tumor therapies

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018187631A1 (en) * 2017-04-05 2018-10-11 Cornell University Trifunctional constructs with tunable pharmacokinetics useful in imaging and anti-tumor therapies

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
NIKKI A THIELE ET AL: "An Eighteen-Membered Macrocyclic Ligand for Actinium-225 Targeted Alpha Therapy", ANGEWANDTE CHEMIE INTERNATIONAL EDITION, vol. 56, no. 46, 13 November 2017 (2017-11-13), Hoboken, USA, pages 14712 - 14717, XP055543785, ISSN: 1433-7851, DOI: 10.1002/anie.201709532 *

Also Published As

Publication number Publication date
KR20190139222A (en) 2019-12-17
US20230372550A1 (en) 2023-11-23
JP7675500B2 (en) 2025-05-13
KR20240093912A (en) 2024-06-24
IL311111A (en) 2024-04-01
EP3600452A1 (en) 2020-02-05
WO2018183906A1 (en) 2018-10-04
AU2018243682B2 (en) 2023-11-09
KR102670305B1 (en) 2024-05-30
NZ757693A (en) 2025-07-25
CN110573186A (en) 2019-12-13
JP2020515596A (en) 2020-05-28
EP4458418A2 (en) 2024-11-06
AU2018243682A1 (en) 2019-10-17
JP2025066780A (en) 2025-04-23
KR20260008174A (en) 2026-01-15
EP3600452A4 (en) 2020-11-18
IL269763B2 (en) 2024-08-01
IL269763A (en) 2019-11-28
CA3058454A1 (en) 2018-10-04
ES2992988T3 (en) 2024-12-20
NZ798439A (en) 2025-08-29
IL269763B1 (en) 2024-04-01
US11554182B2 (en) 2023-01-17
US20210085808A1 (en) 2021-03-25
EP3600452B1 (en) 2024-09-04

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